Protein / target

Integrin beta-3

Encoded byITGB3P05106Homo sapiensSwiss-Prot

UniProt: P05106 Ensembl: ENSG00000259207 HGNC: HGNC:6156 NCBI Gene: 3690

Clinically validated

Therapeutic maturity

Approved medicines

Open Targets target-level

View by indication →

Clinical trials

Small-molecule tractable

Druggability

Approved Drug

Protein at a glance

Biological role

Vascular endothelial growth factor receptor 2 binding

Strongest disease association

Autosomal dominant macrothrombocytopenia

Via encoding gene ITGB3 · Genetic evidence · score 0.78

Therapeutic position

Established drug target

Small molecules and antibodies

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

View complete UniProt function annotation

Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha-V/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha-IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain (By similarity). Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen (PubMed:9111081). This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets (By similarity). ITGAV:ITGB3 binds to fractalkine (CX3CL1) and acts as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887). In brain, plays a role in synaptic transmission and plasticity. Involved in the regulation of the serotonin neurotransmission, is required to localize to specific compartments within the synapse the serotonin receptor SLC6A4 and for an appropriate reuptake of serotonin. Controls excitatory synaptic strength by regulating GRIA2-containing AMPAR endocytosis, which affects AMPAR abundance and composition (By similarity). ITGAV:ITGB3 act as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428). Integrin ITGA2B:ITGB3 is also the receptor of the erythrocyte-specific ICAM4 ligand involved in heterotypic cell-cell adhesion between erythrocytes and activated platelets (PubMed:12477717)

Subcellular location

Cell membraneCell projection, lamellipodium membraneCell junction, focal adhesionPostsynaptic cell membraneSynapse

Domains and Gene Ontology detail (107)

Domains & features

PSIVWFAI-EGF 1I-EGF 2I-EGF 3I-EGF 4

Gene Ontology

Calpha9-beta1 integrin-ADAM8 complex
Calphav-beta3 integrin-HMGB1 complex
Calphav-beta3 integrin-IGF-1-IGF1R complex
Calphav-beta3 integrin-PKCalpha complex
Calphav-beta3 integrin-vitronectin complex
Capical plasma membrane
Ccell surface
Ccell-cell junction
Cexternal side of plasma membrane
Cextracellular exosome
Cfilopodium membrane
Cfocal adhesion

788 aa · 87 kDa · 3 isoforms

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Excitatory neurotransmissionUniProt · GOCell migrationGOLipid & lipoprotein metabolismGOGrowth-factor signallingGOReceptor tyrosine kinase signallingUniProtCell adhesionUniProt · GO

View supporting evidence

Excitatory neurotransmission

·Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin…
·glutamatergic synapse

Cell migration

·cell migration
·negative chemotaxis
·positive regulation of endothelial cell migration
·positive regulation of smooth muscle cell migration

Lipid & lipoprotein metabolism

·apolipoprotein A-I-mediated signaling pathway
·negative regulation of lipid transport
·negative regulation of lipoprotein metabolic process
·negative regulation of low-density lipoprotein particle clearance

Growth-factor signalling

·cellular response to insulin-like growth factor stimulus
·positive regulation of vascular endothelial growth factor receptor signaling pathway

Receptor tyrosine kinase signalling

·Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin…

Cell adhesion

·Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin…
·Cell junction, focal adhesion
·cell-cell junction
·cell adhesion molecule binding

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Approved medicines with mapped indications

2 medicines · 4 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Angina, Unstable2 medicines

abciximab eptifibatide

Thrombosis2 medicines

abciximab eptifibatide

Acute Coronary Syndrome1 medicine

eptifibatide

Myocardial Infarction1 medicine

eptifibatide

4 medicines meet Open Targets' target-level approved-medicine definition; the 2 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

eptifibatide

ApprovedInhibitor

Integrin alpha-IIb/beta-3 inhibitor

Indicated for Acute Coronary Syndrome, Angina, Unstable, Myocardial Infarction, Thrombosis

Acts on a complex — shared with ITGA2B · 1 of 2 recorded protein targets — narrow recorded profile

abciximab

ApprovedInhibitor

Integrin alpha-IIb/beta-3 inhibitor

Indicated for Angina, Unstable, Thrombosis

Acts on a complex — shared with ITGA2B · 1 of 3 recorded protein targets — narrow recorded profile

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene ITGB3

Gene-level evidence surfaced through the gene ITGB3that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Autosomal dominant macrothrombocytopenia

0.82Well supported

Genetic evidence dominant · Open Targets 0.63

Myocardial Infarction

0.70Moderately supported

Clinical evidence dominant · Open Targets 0.57

Acute Coronary Syndrome

0.67Moderately supported

Clinical evidence dominant · Open Targets 0.54

Cardiomyopathy, Hypertrophic

0.52Limited support

Pathway evidence dominant · Open Targets 0.52 · no direct causal or clinical evidence

Neoplasms

0.49Limited support

Pathway evidence dominant · Open Targets 0.62

View evidence synthesis (5)

Autosomal dominant macrothrombocytopeniaWell supported

0.82

agreement 0.70–0.94

Genetic79%Animal model20%Literature1%Genetic literaturedup

Open Targets aggregate 0.63 · 3 independent evidence families · 1 not counted as duplicate

Myocardial InfarctionModerately supported

0.70

agreement 0.55–0.86

Clinical94%Literature6%

Open Targets aggregate 0.57 · 2 independent evidence families

Acute Coronary SyndromeModerately supported

0.67

agreement 0.52–0.83

Clinical98%Literature2%

Open Targets aggregate 0.54 · 2 independent evidence families

Cardiomyopathy, HypertrophicLimited support

0.52

agreement 0.38–0.66

Pathway54%Animal model44%Literature2%

Open Targets aggregate 0.52 · 3 independent evidence families · no direct causal or clinical evidence

NeoplasmsLimited support

0.49

agreement 0.36–0.62

Pathway68%Literature24%Clinical8%

Open Targets aggregate 0.62 · 3 independent evidence families

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations

Autosomal dominant macrothrombocytopenia0.63

Neoplasms0.62

Myocardial Infarction0.57

Acute Coronary Syndrome0.54

Noonan syndrome0.53

Cardiomyopathy, Hypertrophic0.52

Drug development

11 compounds recorded · 4 approved · 7 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 2 drugs that target this protein in Forefront's canonical graph (2 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)

ATN-161Phase 2

TIROFIBAN HYDROCHLORIDEApproval

INTETUMUMABPhase 2

ETARACIZUMABPhase 2

ZALUNFIBANPhase 3

TIROFIBANApproval

EPTIFIBATIDEApproval

ABCIXIMABApproval

TADOCIZUMABPhase 2

ABITUZUMABPhase 2

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small molecules — Strong

Approved Drug and Structure with Ligand support this modality.

Antibodies — Strong

Approved Drug and UniProt loc high conf support this modality.

Protein degraders — Emerging

Feasibility evidence (database ubiquitination and small molecule binder) — no clinical-stage drug of this modality recorded.

Other modalities — Strong

Approved Drug support this modality.

View underlying tractability evidence (13)

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · Approved DrugAB · UniProt loc high confAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMAB · Human Protein Atlas locPR · Database UbiquitinationPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

Clinical trials

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

Efficacy and Safety of Eptifibatide Therapy Following Intravenous Thrombolysis in Acute Ischemic Stroke Patients Within 4.5 to 24 Hours After Onset: A Multicenter, Randomized Controlled TrialPHASE3

NOT_YET_RECRUITING · via eptifibatide · NCT07347626

A Randomized Trial to Compare Four Different Intracoronary Modalities to Reduce Thrombus Burden and Improve Microcirculatory Function in Patients With ST-elevation Myocardial Infarction: Rationale and Design of the COCTAIL II StudyPHASE4

UNKNOWN · via abciximab · NCT01499407

The Effect of Point-of-care Platelet Function Assay Guided Antiplatelet Therapy on the Periprocedural Increase of Cardiac Enzymes.PHASE4

COMPLETED · via abciximab · NCT01475552

A RANDOMIZED TRIAL COMPARING EPTIFIBATIDE AND PLACEBO IN PATIENTS WITH DIFFUSE CORONARY DISEASE UNDERGOING DRUG-ELUTING STENTINGPHASE4

TERMINATED · via eptifibatide · NCT01454440

View all trials (26)

A Randomized Trial of Early Discharge After Trans-radial Stenting of Coronary Arteries in Acute Myocardial Infarction: The EASY-MI Pilot Study.PHASE4

COMPLETED · via abciximab · NCT00440778

A Randomized Trial of Early Discharge After Trans-Radial Stenting of Coronary Arteries in Acute Myocardial Infarction and RESCUE-PCI: The EASY-RESCUE Pilot StudyPHASE4

COMPLETED · via abciximab · NCT00440895

Routine Upfront Abciximab Versus Standard Peri-Procedural Therapy in Patients Undergoing Percutaneous Coronary Intervention for Cardiogenic Shock PRAGUE-7 Trial.PHASE4

COMPLETED · via abciximab · NCT00420030

A Randomized Trial Comparing the Efficacy on Myocardial Infarct Size Reduction of Early vs. Late Abciximab Administration During Primary Percutaneous Coronary AngioplastyPHASE4

COMPLETED · via abciximab · NCT00354406

Research Evaluation to Study Individuals Who Show Thromboxane Or P2Y12 Receptor ResistancePHASE4

TERMINATED · via eptifibatide · NCT00289601

A Comparison of Drug Eluting and Bare Metal Stents With or Without Abciximab in ST Segment Elevation Myocardial Infarction The Eindhoven Reperfusion StudyPHASE4

COMPLETED · via abciximab · NCT00986050

Clinical Effects of Eptifibatide Administration in High Risk Patients Presenting With Non-ST Segment Elevation Acute Coronary Syndrome (NSTE-ACS) Requiring Urgent Coronary Artery Bypass Graft Surgery in Short- and Long-Term Follow-upPHASE4

COMPLETED · via eptifibatide · NCT01863134

Brief Infusion of Eptifibatide Following Percutaneous Coronary InterventionPHASE4

COMPLETED · via eptifibatide · NCT00111566

Half-Dose Intracoronary Abciximab Bolus Improves the Mortality Outcome Compared to Standard Intravenous RegimenPHASE4

TERMINATED · via abciximab · NCT00320229

A Randomized Trial Comparing Same Day Discharge and a Single Bolus of Abciximab to Overnight Hospitalization and Bolus + Perfusion Abciximab After Uncomplicated Trans-Radial Coronary Artery StentingPHASE4

COMPLETED · via abciximab · NCT00169819

Value of Abciximab in Patients With AMI Undergoing PCI After High Dose Clopidogrel Pretreatment (BRAVE 3)PHASE4

COMPLETED · via abciximab · NCT00133250

FATA: Comparison Between Tirofiban and Abciximab in Facilitated Angioplasty With Stent Implantation: Randomized Multicentre StudyPHASE4

COMPLETED · via abciximab · NCT00383136

Prospective, Randomized, Double-Blind, Placebo-Controlled Trial of the Glycoprotein IIb/IIIa Inhibition With Abciximab in Patients With ACS Undergoing Coronary Stenting After Pretreatment With a High Loading Dose of Clopidogrel (ISAR-REACT-2)PHASE4

COMPLETED · via abciximab · NCT00133003

Multi-arm Optimization of Stroke Thrombolysis (MOST): a Single Blinded, Randomized Controlled Adaptive, Multi-arm, Adjunctive-thrombolysis Efficacy Trial in Ischemic StrokePHASE3

COMPLETED · via eptifibatide · NCT03735979

Safety and Efficacy of Eptifibatide in Endovascular Treatment of Acute Ischemic Stroke: a Single-arm, Open-label, Multicenter Clinical TrialPHASE3

UNKNOWN · via eptifibatide · NCT03844594

Randomized, Double-blind, Triple-dummy Trial to Compare the Efficacy of Otamixaban With Unfractionated Heparin + Eptifibatide, in Patients With Unstable Angina/Non ST Segment Elevation Myocardial Infarction Scheduled to Undergo an Early Invasive StrategyPHASE3

COMPLETED · via eptifibatide · NCT01076764

IntraCoronary Abciximab With the ClearWay Catheter To Improve Outcomes With LysisPHASE3

TERMINATED · via abciximab · NCT00894023

INSTANT: INtegrilin Plus STenting to Avoid Myocardial Necrosis TrialPHASE3

COMPLETED · via eptifibatide · NCT00638976

Eptifibatide Versus Abciximab in Primary PCI for Acute ST Elevation Myocardial InfarctionPHASE3

COMPLETED · via abciximab · NCT00426751

Does Abciximab Save Hypoperfused Ischemic Brain Tissue in Wake-Up Stroke: A Placebo-Controlled, Randomized, MR Imaging StudyPHASE3

TERMINATED · via abciximab · NCT00167765

Myocardial Infarction With ST-elevation Treated by Primary Percutaneous Intervention Facilitated by Early Reopro Administration in Alsace.PHASE3

UNKNOWN · via abciximab · NCT00638638

Early Glycoprotein IIb/IIIa Inhibition in Non-ST-segment Elevation Acute Coronary Syndrome: A Randomized, Placebo-Controlled Trial Evaluating the Clinical Benefits of Early Front-loaded Eptifibatide in the Treatment of Patients With Non-ST-segment Elevation Acute Coronary Syndrome (EARLY ACS)PHASE3

COMPLETED · via eptifibatide · NCT00089895

Abciximab Versus Aspirin for Prevention of Stroke Recurrence Before Endarterectomy in Symptomatic >50% Carotid Stenosis: A Pilot Study (ASTERICS)PHASE3

TERMINATED · via abciximab · NCT00126139

Abciximab (ReoPro) in Acute Ischemic Stroke: A Phase III, Multinational, Multicenter, Randomized, Double-blind, Placebo-controlled Trial.PHASE3

TERMINATED · via abciximab · NCT00073372

ReoPro and Peripheral Arterial Intervention to Improve Clinical Outcome in Patients With Peripheral Arterial Disease - A Randomized Prospective Trial (RIO-Trial)PHASE2/PHASE3

UNKNOWN · via abciximab · NCT00156611

A Phase IIIb, Randomised, Open Label Trial With 3 Parallel Groups: Full Dose TNK-tPA Together With Heparin Sodium, Full Dose TNK-tPA Together With Enoxaparin, and Half Dose TNK-tPA Together With Abciximab and Heparin Sodium in Patients With Acute Myocardial Infarction: ASSENT 3 (Assessment of the Safety and Efficacy of New Thrombolytic Regimens)PHASE3

COMPLETED · via abciximab · NCT02181985

ClinicalTrials.gov via the drug-target graph.

What's happening now

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

Withdrawn from market2026-01-01
Market withdrawal: Integrilin (EMA)
ema · market · ema · via eptifibatide
Regulatory approval2016-01-11
Approval: Eptifibatide Accord (EMA)
ema · regulatory · ema · via eptifibatide
New publication2015-08-04
Combined Approach to Lysis Utilizing Eptifibatide and Recombinant Tissue-Type Plasminogen Activator in Acute Ischemic Stroke-Full Dose Regimen Stroke Trial.
Stroke · 2015 · 52 citations · Europe PMC · via eptifibatide
New publication2009-03-01
Abbreviated infusion of eptifibatide after successful coronary intervention The BRIEF-PCI (Brief Infusion of Eptifibatide Following Percutaneous Coronary Intervention) randomized trial.
Journal of the American College of Cardiology · 2009 · 40 citations · Europe PMC · via eptifibatide
New publication2007-11-21
Emergency administration of abciximab for treatment of patients with acute ischemic stroke: results of an international phase III trial: Abciximab in Emergency Treatment of Stroke Trial (AbESTT-II).
Stroke · 2008 · 234 citations · Europe PMC · via abciximab
New publication1999-04-01
Sustained suppression of ischemic complications of coronary intervention by platelet GP IIb/IIIa blockade with abciximab: one-year outcome in the EPILOG trial. Evaluation in PTCA to Improve Long-term Outcome with abciximab GP IIb/IIIa blockade.
Circulation · 1999 · 72 citations · Europe PMC · via abciximab

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.